Ilaprazole (IY-81149) sodium,一种具有口服活性质子泵抑制剂,以剂量依赖性方式不可逆地抑制H+/K+-ATPase,在兔壁细胞制剂中的IC50为 6 μM。Ilaprazole sodium 用于胃溃疡的研究。Ilaprazole sodium 也是一种有效的T细胞起源蛋白激酶(TOPK)抑制剂。
生物活性 | Ilaprazole (IY-81149) sodium is an orally activeproton pumpinhibitor. Ilaprazole sodium irreversibly inhibitsH+/K+-ATPasein a dose-dependent manner with anIC50of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potentTOPK(T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2]. |
体外研究 (In Vitro) | On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50of Ilaprazole (IY-81149) sodium is 9 nM[1].
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体内研究 (In Vivo) | Ilaprazole sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion[1]. In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED50of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50is 2.1 mg/kg and that of Omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium is equipotent to Omeprazole. Ilaprazole sodium also inhibits gastric acid secretion strongly in fistular rats. The ED50of Ilaprazole sodium administered intraduodenally is 0.43 mg/kg and that of omeprazole Is 0.68 mg/kg[1].
Animal Model: | Male SD rat (after pylorus ligation)[1] | Dosage: | 3, 10, 30 mg/kg | Administration: | Intraduodenally | Result: | The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 41.67 mg/mL(107.28 mM;Need ultrasonic) 配制储备液 1 mM | 2.5745 mL | 12.8727 mL | 25.7453 mL | 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL | 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.36 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.36 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.36 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.36 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.36 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.36 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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